Synthesis, Characterization, Genotoxicity Assessment and Biological Activity of Derivatives Derived from Flucytosine Drug

Because pyrimidine compounds contain two nitrogen atoms in the ring, their structures are a class of significant organic compounds that include hetero atoms. These groups are thought to be the previously derivatives with pharmacological and biological activities toward many types of pathogenic organisms. To study the antimicrobial activity of three different types of derivatives (C۱, C۲, and C۳) against two different species of bacteria (Escherichia coli and Proteus vulgaris) and two different species of fungi (Aspergillus niger and Penicillium chrysogenum), the derivatives have been prepared at three different concentrations (۱۰, ۱۵, and ۲۰ mg/mL). The results showed that three derivatives had antimicrobial activity at all studied concentrations, but the best antibacterial and antifungal effect was recorded at the concentration (۲۰ mg/mL) against all microbial isolates studied. Furthermore, in vivo genotoxicity of two compounds (C۲ and C۳) was investigated in rats using the ۸-hydroxy-۲۰-deoxyguanosine (۸-OHdG) assay. In addition, when rats were treated with ۵۰۰ mg/kg body weight of compound C۳, there was a considerable suppression of the urine ۸-OHdG level (۵۰.۲%) (p < ۰.۰۰۰۱). Compound C۲, however, raised the amounts of ۸-OHdG in the urine. Using an up-and-down method to calculate the fatal dosage (LD۵۰) values for compounds C۲ and C۳, it was shown that these compounds are safe because the LD۵۰ was greater than ۱۰۰۰ mg/kg" b.w". Because the studied compounds have strong antibacterial activity and low genotoxicity, they may find application as antibiotics.

کلیدواژه ها:

Pyrimidine ، azomethine ، Flucytosine drug ، Biological activity ، genotoxicity